856875-79-1Relevant academic research and scientific papers
COMPOSITIONS AND METHODS FOR THE TREATMENT OF MALARIA
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Page/Page column 80; 83, (2014/10/15)
The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.
Evaluation of aminohydantoins as a novel class of antimalarial agents
Meyers, Marvin J.,Tortorella, Micky D.,Xu, Jing,Qin, Limei,He, Zhengxiang,Lang, Xingfen,Zeng, Wentian,Xu, Wanwan,Qin, Li,Prinsen, Michael J.,Sverdrup, Francis M.,Eickhoff, Christopher S.,Griggs, David W.,Oliva, Jonathan,Ruminski, Peter G.,Jacobsen, E. Jon,Campbell, Mary A.,Wood, David C.,Goldberg, Daniel E.,Liu, Xiaorong,Lu, Yongzhi,Lu, Xin,Tu, Zhengchao,Lu, Xiaoyun,Ding, Ke,Chen, Xiaoping
supporting information, p. 89 - 93 (2014/02/14)
Given the threat of drug resistance, there is an acute need for new classes of antimalarial agents that act via a unique mechanism of action relative to currently used drugs. We have identified a set of druglike compounds within the Tres Cantos Anti-Malar
Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
Cumming, Jared N.,Smith, Elizabeth M.,Wang, Lingyan,Misiaszek, Jeffrey,Durkin, James,Pan, Jianping,Iserloh, Ulrich,Wu, Yusheng,Zhu, Zhaoning,Strickland, Corey,Voigt, Johannes,Chen, Xia,Kennedy, Matthew E.,Kuvelkar, Reshma,Hyde, Lynn A.,Cox, Kathleen,Favreau, Leonard,Czarniecki, Michael F.,Greenlee, William J.,McKittrick, Brian A.,Parker, Eric M.,Stamford, Andrew W.
, p. 2444 - 2449 (2012/05/19)
From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived Aβ following oral administration to rats. Herein we report SAR development in the S3 and F′ subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound.
